2型糖尿病药物磷酸西他列汀的合成  

Synthesis of the type 2 anti-diabetic drug sitagliptin phosphate

作　　者：吕承林 沈方亮 孙鑫哲[1] 张兴贤[1] 

机构地区：[1]浙江工业大学药学院,杭州310032

出　　处：《中国新药杂志》2014年第13期1574-1578,共5页Chinese Journal of New Drugs

基　　金：国家级大学生创新创业训练计划(201210337009)

摘　　要：目的:研究磷酸西他列汀的合成新方法。方法:以2,4,5-三氟苯乙酸和2,2-二甲基-1,3-二噁烷-4,6-二酮为起始原料经10步反应合成了目标产物磷酸西他列汀。结果与结论:目标产物结构经1H-NMR,13CNMR和EI-MS确证,总产率为33%。该合成路线具有原料价廉易得、反应条件温和、收率高的特点,具有较好的工业化应用前景。Objective： To investigate the new synthetic method of sitagliptin phosphate, a type Ⅱ anti-diabetic drug. Methods ： Using 2,4,5-trifluorophenylacetic acid and 2,2-dimethyl-1,3-dioxane-4,6-dione as starting materials, sitagliptin phosphate was synthesized through 10 steps. Results and Conclusion： The structure of target product was characterized by ^1H-NMR, ^13C-NMR and EI-MS. The overall yield was 33%. This synthetic method has advantages such as cheap and easily available material, mild reaction conditions, high yield and simple operation, which is suitable for the large-scale production.

关 键 词：磷酸西他列汀 抗糖尿病药物 手性中间体 不对称合成 

分 类 号：R914.5[医药卫生—药物化学]